Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors.
Annu Rev Pharmacol Toxicol
; 60: 89-107, 2020 01 06.
Article
em En
| MEDLINE
| ID: mdl-31454292
ABSTRACT
Recent advances in our understanding of the structure and function of class B G protein-coupled receptors (GPCRs) provide multiple opportunities for targeted development of allosteric modulators. Given the pleiotropic signaling patterns emanating from these receptors in response to a variety of natural agonist ligands, modulators have the potential to sculpt the responses to meet distinct needs of different groups of patients. In this review, we provide insights into how this family of GPCRs differs from the rest of the superfamily, how orthosteric agonists bind and activate these receptors, the potential for allosteric modulators to interact with various regions of these targets, and the allosteric influence of endogenous proteins on the pharmacology of these receptors, all of which are important considerations when developing new therapies.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Acoplados a Proteínas G
/
Regulação Alostérica
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Desenvolvimento de Medicamentos
Limite:
Humans
Idioma:
En
Revista:
Annu Rev Pharmacol Toxicol
Ano de publicação:
2020
Tipo de documento:
Article